RESUMO
Irreversible loss of retinal ganglion cells (RGCs) is a common pathological feature of various optic nerve degenerative diseases such as glaucoma and ischemic optic neuropathy. Effective protection of RGCs is the key to successful treatment of these diseases. Total Panax notoginseng saponins (TPNS) are the main active component of Panax notoginseng, which has an inhibitory effect on the apoptosis pathway. This study is aimed at assessing the protective effect of TPNS on RGCs of the optic nerve crush (ONC) model of rats and exploring the underlying mechanisms. The intraperitoneal or intravitreal injection of TPNS was used based on the establishment of the rat ONC model. Fifteen days after the injury, the cell membrane fluorescent probe (Fluoro-Gold) was applied to retrograde RGCs through the superior colliculus and obtain the number of surviving RGCs. TUNEL assay was also used to detect the number and density of RGC apoptosis after the ONC model. The expression and distribution of Bcl-2/Bax, c-Jun/P-c-Jun, and P-JNK in the retina were demonstrated by Western blot analysis. After the intervention of TPNS, the rate of cell survival increased in different retinal regions (p < 0.05) and the number of apoptosis cells decreased. Regarding the expression of Bcl-2/Bax, c-Jun/P-c-Jun, and P-JNK-related apoptotic proteins, TPNS can reduce the level of apoptosis and play a role in protecting RGCs (p < 0.05). These findings indicate that topical administration of TPNS can inhibit cell apoptosis and promote RGC survival in the crushed optic nerve.
Assuntos
Lesões por Esmagamento/tratamento farmacológico , Traumatismos do Nervo Óptico/tratamento farmacológico , Panax notoginseng/química , Células Ganglionares da Retina/efeitos dos fármacos , Saponinas/administração & dosagem , Animais , Apoptose , Biomarcadores/metabolismo , Sobrevivência Celular , Modelos Animais de Doenças , Regulação da Expressão Gênica/efeitos dos fármacos , Injeções Intraperitoneais , Injeções Intravítreas , Masculino , Traumatismos do Nervo Óptico/metabolismo , Extratos Vegetais/administração & dosagem , Extratos Vegetais/farmacologia , Ratos , Células Ganglionares da Retina/metabolismo , Saponinas/farmacologia , Resultado do TratamentoRESUMO
BACKGROUND Chronic ocular hypertension (COH) models mostly focus on changes in intraocular pressure (IOP) and loss of retinal ganglion cells (RGCs). The present study evaluated important glaucoma-related changes in visual function, response to common ocular hypotensive drugs, and safety for our previously developed rat model. MATERIAL AND METHODS The model was established through a single injection of hydrogel into the anterior chambers. Efficacy was assessed through F-VEP by measuring latency and amplitude of P1. We evenly divided 112 rats into 4 groups: control and COH at 2, 4, and 8 weeks. Response to 5 common drugs (brimonidine, timolol, benzamide, pilocarpine, and bimatoprost) were each tested on 6 rats and assessed using difference in IOP. Safety assessment was conducted through histological analysis of 24 rats evenly divided into 4 groups of control and COH at 2, 4, and 8 weeks. Corneal endothelial cells (CECs) of 24 additional rats were used to determine toxic effects through TUNEL and CCK-8 assays. RESULTS P1 latency and amplitude of VEP demonstrated the model is effective in inducing optic nerve function impairment. Only the drug pilocarpine failed to have an obvious hypotensive effect, while the other 4 were effective. CECs at 2, 4, and 8 weeks showed no significant differences from control groups in results of histological analysis, TUNEL, and CCK-8 assays. CONCLUSIONS A single injection of hydrogel into the anterior chamber is effective for modeling COH, can respond to most commonly used hypotensive drugs, and is non-toxic to the eyes.
Assuntos
Anti-Hipertensivos/farmacologia , Hidrogéis/efeitos adversos , Pressão Intraocular/efeitos dos fármacos , Hipertensão Ocular , Animais , Doença Crônica , Modelos Animais de Doenças , Avaliação Pré-Clínica de Medicamentos , Hidrogéis/farmacologia , Masculino , Hipertensão Ocular/induzido quimicamente , Hipertensão Ocular/tratamento farmacológico , Hipertensão Ocular/fisiopatologia , Ratos , Ratos Sprague-DawleyRESUMO
Three new phenolic compounds (1-3) were isolated from the heartwood of Dalbergia odorifera T. Chen. (Leguminosae). Their structures were established based on spectroscopic methods including 1D and 2D NMR (HSQC, COSY, HMBC and ROESY). Compound 2 exhibited cytotoxicity against BEL-7402 tumor cell lines.
Assuntos
Antineoplásicos Fitogênicos/isolamento & purificação , Benzofuranos/isolamento & purificação , Cromonas/isolamento & purificação , Dalbergia/química , Medicamentos de Ervas Chinesas/isolamento & purificação , Flavonoides/isolamento & purificação , Compostos Heterocíclicos de 4 ou mais Anéis/isolamento & purificação , Antineoplásicos Fitogênicos/química , Antineoplásicos Fitogênicos/farmacologia , Benzofuranos/química , Benzofuranos/farmacologia , Cromonas/química , Cromonas/farmacologia , Ensaios de Seleção de Medicamentos Antitumorais , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/farmacologia , Flavonoides/química , Flavonoides/farmacologia , Compostos Heterocíclicos de 4 ou mais Anéis/química , Compostos Heterocíclicos de 4 ou mais Anéis/farmacologia , Humanos , Estrutura Molecular , Ressonância Magnética Nuclear Biomolecular , Fenóis/químicaRESUMO
Fourteen compounds were isolated from Dalbergia odoriferae and purified by repeated column chromatography on silica and sephadex LH-20 gel and structurally identified by spectral analysis. These compounds were identified as 4, 9-dimethoxy-3-hydroxypterocarpan (1), medicarpin (2), 2', 4', 5-trihydroxy-7-methoxyisoflavone (3), 2', 3', 7-trihydroxy-4'-methoxyisoflavan (4), formononetin (5), 3, 8-dihydroxy-9-methoxypterocarpan (6), koparin (7), 3-hydroxy-9-methoxypterocarp-6a-ene (8), 2'-hydroxyformononetin (9), stevenin (10), 2', 7-dihydroxy-4', 5'-dimethoxyisoflavone (11), lyoniresinol (12), 2, 4-dihydroxy-5-methoxy-benzophenone (13) and neokhriol A (14). Compounds 1, 3, 4, 6, 8, 12 and 14 were isolated from this plant for the first time. Antibacterial activity assay showed that compound 4 had inhibitory effect on Ralstonia solanacearum.
Assuntos
Dalbergia/química , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Anisóis/química , Anisóis/isolamento & purificação , Anisóis/farmacologia , Antibacterianos/química , Antibacterianos/isolamento & purificação , Antibacterianos/farmacologia , Benzofenonas/química , Benzofenonas/isolamento & purificação , Benzofenonas/farmacologia , Cromatografia/métodos , Dextranos , Géis , Isoflavonas/química , Isoflavonas/isolamento & purificação , Isoflavonas/farmacologia , Testes de Sensibilidade Microbiana , Naftalenos/química , Naftalenos/isolamento & purificação , Naftalenos/farmacologia , Extratos Vegetais/farmacologia , Pterocarpanos/química , Pterocarpanos/isolamento & purificação , Pterocarpanos/farmacologia , Ralstonia solanacearum/efeitos dos fármacos , Ralstonia solanacearum/crescimento & desenvolvimento , Sílica GelRESUMO
Five new sesquiterpenes (1-5) along with ten known ones were isolated from the heartwood of Dalbergia odorifrea T. Chen. Their structures were determined by spectroscopic techniques including MS, UV, IR, 1D and 2D NMR. Bioassay results showed that compounds 1 and 9 had inhibitory effect on Candida albicans, and compound 9 exhibited inhibitory effects on Staphylococcus aureus by paper disk diffusion method.
Assuntos
Candida albicans/efeitos dos fármacos , Dalbergia/química , Estrutura Molecular , Extratos Vegetais/farmacologia , Sesquiterpenos/farmacologia , Staphylococcus aureus/efeitos dos fármacos , Espectroscopia de Ressonância Magnética , Medicina Tradicional Chinesa , Extratos Vegetais/química , Extratos Vegetais/isolamento & purificação , Plantas Medicinais , Sesquiterpenos/química , Sesquiterpenos/isolamento & purificação , Madeira/químicaRESUMO
AIM: To study the chemical constituents of the whole plant of Chloranthus japonicus. METHODS: Compounds were isolated and purified by column chromatography. Their structures were elucidated on the basis of spectroscopic methods. RESULTS: Six sesquiterpenoids were obtained and their structures were identified as chlojaponilactone A (1), atractylenolide III (2), neolitacumone B (3), 10α-hydroxy-1-oxoeremophila-7(11), 8(9)-diene-8, 12-olide (4), shizukanolide C (5), and shizukanolide H (6). CONCLUSION: Compound 1 is a new eudesmane-type sesquiterpenoid lactone, and compounds 3 and 4 have been isolated from this species for the first time.
Assuntos
Magnoliopsida/química , Extratos Vegetais/química , Sesquiterpenos/isolamento & purificação , Estrutura Molecular , Sesquiterpenos/químicaRESUMO
A new flavonolignan, anthelminthicol A (1), together with four known compounds, was isolated from the EtOAc extracts of the seeds of Hydnocarpus anthelminthica. Their structures were elucidated using extensive spectroscopic techniques. Bioassay showed that compounds 3-5 could inhibit nitric oxide production in LPS-stimulated RAW 264.7 macrophage cell lines, with IC(50) values of 7.81, 9.38, and 10.55 µM, respectively.
Assuntos
Anti-Inflamatórios não Esteroides/isolamento & purificação , Anti-Inflamatórios não Esteroides/farmacologia , Medicamentos de Ervas Chinesas/isolamento & purificação , Medicamentos de Ervas Chinesas/farmacologia , Flavonolignanos/isolamento & purificação , Flavonolignanos/farmacologia , Salicaceae/química , Animais , Anti-Inflamatórios não Esteroides/química , Dinoprostona/farmacologia , Medicamentos de Ervas Chinesas/química , Flavonolignanos/química , Lipopolissacarídeos/farmacologia , Macrófagos/efeitos dos fármacos , Camundongos , Estrutura Molecular , Óxido Nítrico/biossíntese , Óxido Nítrico/farmacologia , Ressonância Magnética Nuclear Biomolecular , Sementes/químicaRESUMO
OBJECTIVE: To establish the HPLC-fingerprint of the water-soluble constituents of Carthamus tinctorius. METHODS: 18 samples of Carthamus tinctorius from different producing areas were determined by Agilent 1100 DAD-HPLC under the chromatographic conditions: column by SinoChrom ODS-BP (250 mm x 4.6 mm, 5 microm), methanol-0.7% H3PO4 water with gradient elution, column temperature 30 degrees C, flow rate by 1 ml/min, wavelength 280 nm, and inject volume 20 microl. RESULTS: The HPLC-fingerprint of the water-soluble constituents of Cartharnus tinctorius was established on the basis of 10 bitch of drugs from Xinjiang according to SPSS analysis. CONCLUSION: A reliable method is provided for the quality identification of Carthamus tinctorius.
Assuntos
Carthamus tinctorius/química , Chalcona/química , Cromatografia Líquida de Alta Pressão/métodos , Plantas Medicinais/química , Carthamus tinctorius/classificação , Chalcona/análise , Chalcona/isolamento & purificação , Análise por Conglomerados , Medicamentos de Ervas Chinesas/química , Medicamentos de Ervas Chinesas/isolamento & purificação , Medicamentos de Ervas Chinesas/normas , Flores/química , Controle de Qualidade , Reprodutibilidade dos TestesRESUMO
A new steroidal saponin, paridiformoside B (1), was obtained from the EtOH extract of the whole plant of Lysimachia Paridiformis Franch, togerher with one steroidal sapogenin (7) and seven known steroidal saponins (2-6, 8-9). Their structures were elucidated using extensive spectroscopic techniques including 1D and 2D NMR spectra.